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Letrozole

InhA, Func 112809-51-5
Catalog No. ABIN4874409
  • Application
    Inhibition Assay (InhA), Functional Studies (Func)
    Purpose
    Letrozole (INN, trade name Femara®) is an oral non-steroidal aromatase inhibitor that has been introduced for the adjuvant treatment of hormonally-responsive breast cancer Estrogens are produced by the conversion of androgens through the activity of the aromatase enzyme. Letrozole blocks production of estrogens in this way by competitive, reversible binding to the heme of its cytochrome P450 unit. The action is specific, and letrozole does not reduce production of mineralo- or corticosteroids. In contrast, the antiestrogenic action of tamoxifen, the major medical therapy prior to the arrival of aromatase inhibitors, is due to its interfering with the estrogen receptor, rather than inhibiting estrogen production. Letrozole is approved by the United States Food and Drug Administration (FDA) for the treatment of local or metastatic breast cancer that is hormone receptor positive or has an unknown receptor status in postmenopausal women. Side effects include signs and symptoms of hypoestrogenism. There is concern that long term use may lead to osteoporosis, which is why prescriptions of Letrozole are often accompanied by prescriptions of osteoporosis-fighting medication such as Fosamax. Letrozole has shown to reduce estrogen levels by 98 percent while raising testosterone levels. The anti-estrogen action of letrozole is preferred by athletes and bodybuilders for use during a steroid cycle to reduce bloating due to excess water retention and prevent the formation of gynecomastia related breast tissue that is a side effect of some anabolic steroids. Usage above 2.5 mg/day is known to potentially temporarily kill sex drive. Above 5mg/day for extended periods may cause kidney problems. Letrozole has also been shown to delay the fusing of the growth plates in adolescents. This may boost the effectiveness of growth hormone, and thus Letrozole is used to treat adolescents and children with short stature.
    Characteristics
    Tradename: FEMARA
    Source of Compound: synthetic
    Target: Aromatase Inhibitor
    Receptor: Aromatase
    Purification
    All the products are sent with COA, HPLC and NMR inspection report to guarantee the quality.
    Purity
    98 %
    Formula
    C17H11N5
    Solubility
    Soluble in water
  • Application Notes
    Optimal working dilution should be determined by the investigator.
    Restrictions
    For Research Use only
  • Format
    Solid
    Storage
    -20 °C
    Storage Comment
    For the majority of compounds, they could be dissolved in DMSO or other organic solvent.
    Their stock solution can be stored at -20°C for up to 3 months and aliquoted for sampling convenience.
    Several freeze/thaw cycles should not damage the activity of our small molecule products.
    However, in many instances the aqueous solutions of some compounds need to be made fresh and cannot be stored. For these compounds, their solution should be prepared just before use and stored no longer than 24 hours.
    Expiry Date
    24 months
  • Background
    Endocrinology/ Hormones
    Molecular Weight
    285.30 g/mol
    CAS-No
    112809-51-5
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